Synthesis and biological evaluations of new nitric oxide-anti-inflammatory drug hybrids

被引：16

作者：

Abdelall, Eman K. A. ^{[1
]}

Abdelhamid, Abdou O. ^{[2
]}

机构：

[1] Beni Suef Univ, Dept Pharmaceut Organ Chem, Fac Pharm, Bani Suwayf 62514, Egypt

[2] Cairo Univ, Dept Chem, Fac Sci, Giza 12613, Egypt

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2017年 / 27卷 / 18期

关键词：

Nitric oxide donor; Diarylpyrazoles; Hydroximoylchloride; 1,3-Dipolar cycloaddition; 2D NMR; Anti-inflammatory; PYRAZOLE CYCLIZATION; CELECOXIB ANALOGS; DERIVATIVES; INHIBITORS; CYCLOOXYGENASE-2; LIABILITY; NO;

D O I：

10.1016/j.bmcl.2017.08.023

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

Three novel series of nitroso derivatives (11-15), isoxazolopyrazoles (17a-c) and isoxazolo[3,4-d]pyridazines (18a-c) were prepared from the hydroxyimoyl chloride 10. In vitro COX1\2 inhibition activities were evaluated, both of 17b and 18a proved a promising inhibitory activity with IC50 = 1.12, 0.78 mu M in sequent. Carrageenan induced Paw edema, ulcer liability, nitric oxide (NO center dot) release and histopathological study were determined. Most of the prepared compounds showed excellent activities. Reactions of 2-aminopyridine and enaminone with hydroxyimoyl chloride 10 were investigated and proved by 2D NMR. Molecular docking for most active compounds was operated giving a hint for compound-receptor interactions. (C) 2017 Elsevier Ltd. All rights reserved.

引用

页码：4358 / 4369

页数：12

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